Diosmetin, also known as 3´, 5, 7-trihydroxy-4´-methoxyflavone, is a bioflavonoid that can be found in several food sources. These include mainly citrus fruits and plants, such as Rosmarinus officinalis, Citrus sinensis, Galium verum, and Rosa agrestis. It has been shown that diosmetin has pharmacological actions that include neuroprotective, antioxidant, and anticancer properties. The objective of this manuscript is to provide a comprehensive review of the pharmacological, pharmacokinetic, and toxicological profile of diosmetin. The information has been collected from several research papers found in various databases, including Web of Science, Pubmed, Scopus, and ScienceDirect. Diosmetin has the potential to reduce inflammation, and it can also improve vascular functions and protect against oxidative stress, both of which are essential for the prevention and management of several diseases.